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Ras proteins as therapeutic targets.
Chakraborty A, Linnane E, Ross S. Chakraborty A, et al. Biochem Soc Trans. 2018 Oct 19;46(5):1303-1311. doi: 10.1042/BST20170529. Epub 2018 Aug 28. Biochem Soc Trans. 2018. PMID: 30154091 Review.
Specific targeting of the KRAS mutational landscape in myeloma as a tool to unveil the elicited antitumor activity.
Sacco A, Federico C, Todoerti K, Ziccheddu B, Palermo V, Giacomini A, Ravelli C, Maccarinelli F, Bianchi G, Belotti A, Ribolla R, Favasuli V, Revenko AS, Macleod AR, Willis B, Cai H, Hauser J, Rooney C, Willis SE, Martin PL, Staniszewska A, Ambrose H, Hanson L, Cattaneo C, Tucci A, Rossi G, Ronca R, Neri A, Mitola S, Bolli N, Presta M, Moschetta M, Ross S, Roccaro AM. Sacco A, et al. Blood. 2021 Nov 4;138(18):1705-1720. doi: 10.1182/blood.2020010572. Blood. 2021. PMID: 34077955 Free PMC article.
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W. Kettle JG, et al. J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26. J Med Chem. 2022. PMID: 35471939
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X. Kettle JG, et al. J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13. J Med Chem. 2020. PMID: 32023060
97 results